Synthesis and evaluation of terbenzimidazoles as topoisomerase I inhibitors

Qun Sun, Barbara Gatto, Chiang Yu, Angela Liu, Leroy-Fong Liu, Edmond J. LaVoie

Research output: Contribution to journalArticle

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Abstract

The synthesis and pharmacological activity of a series of terbenzimidazoles are described. The ability of these derivatives to induce DNA cleavage in the presence of topoisomerase I was evaluated in vitro. These analogs were also assayed for their cytotoxicity in RPMI 8402 cells and the camptothecin-resistant CPT-K5 cells. In addition the potential for these compounds to serve as substrates for MDR1 was also determined. Several terbenzimidazoles exhibited similar cytotoxicity against variants of human tumor cells that either overexpress MDR1 or are camptothecin-resistant.

Original languageEnglish
Pages (from-to)3638-3644
Number of pages7
JournalJournal of Medicinal Chemistry
Volume38
Issue number18
Publication statusPublished - 1995
Externally publishedYes

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Topoisomerase I Inhibitors
Camptothecin
Cytotoxicity
Type I DNA Topoisomerase
Tumors
DNA Cleavage
Cells
Derivatives
DNA
Substrates
Pharmacology
Neoplasms

ASJC Scopus subject areas

  • Organic Chemistry

Cite this

Sun, Q., Gatto, B., Yu, C., Liu, A., Liu, L-F., & LaVoie, E. J. (1995). Synthesis and evaluation of terbenzimidazoles as topoisomerase I inhibitors. Journal of Medicinal Chemistry, 38(18), 3638-3644.

Synthesis and evaluation of terbenzimidazoles as topoisomerase I inhibitors. / Sun, Qun; Gatto, Barbara; Yu, Chiang; Liu, Angela; Liu, Leroy-Fong; LaVoie, Edmond J.

In: Journal of Medicinal Chemistry, Vol. 38, No. 18, 1995, p. 3638-3644.

Research output: Contribution to journalArticle

Sun, Q, Gatto, B, Yu, C, Liu, A, Liu, L-F & LaVoie, EJ 1995, 'Synthesis and evaluation of terbenzimidazoles as topoisomerase I inhibitors', Journal of Medicinal Chemistry, vol. 38, no. 18, pp. 3638-3644.
Sun, Qun ; Gatto, Barbara ; Yu, Chiang ; Liu, Angela ; Liu, Leroy-Fong ; LaVoie, Edmond J. / Synthesis and evaluation of terbenzimidazoles as topoisomerase I inhibitors. In: Journal of Medicinal Chemistry. 1995 ; Vol. 38, No. 18. pp. 3638-3644.
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